indoxyl sulfate potassium

Potassium 1H-indol-3-yl sulfate (Potassium 3-indoxyl sulfate) 是人芳烃受体(AhR)的激动剂。芳烃受体(AhR)最近被发现是免疫炎症条件的病理生理调节剂，Potassium 1H-indol-3-yl sulfate 已被证明是AhR的配体。Potassium 1H-indol-3-yl sulfate 也是膳食蛋白质中色氨酸的代谢物。色氨酸被肠道细菌代谢为吲哚，吲哚被吸收到血液中，然后在肝脏中进一步代谢为硫酸吲哚，通常通过尿液排出体外。在肾功能受损的慢性肾病患者中，Potassium 1H-indol-3-yl sulfate 可作为尿毒症毒素在血清中积累，诱导氧化应激并加速疾病进展。250 μM Potassium 1H-indol-3-yl sulfate 可诱导NF-Κb活化，促进大鼠近端小管细胞TGF-β1和Smad3的表达，与促纤维化活性相关。

Indoxyl sulfate-d5 is intended for use as an internal standard for the quantification of indoxyl sulfate by GC- or LC-MS. Indoxyl sulfate is a uremic toxin and a metabolite of tryptophan. It is formed via sulfation of indole, an intermediate generated from tryptophan by intestinal bacteria, by the sulfotransferase (SULT) isoform 1A1 variant 2 (SULT1A1*2) in the liver. Indoxyl sulfate activates the aryl hydrocarbon receptor (AhR) in HepG2 40 6 hepatoma cells (EC50 = 12.1 nM in a reporter assay). It also inhibits the organic anion transporter (OAT) isoforms OAT1 and OAT3 (Kis = 34.2 and 74.4 µM, respectively for the rat transporters) in S2 proximal tubule cells. Indoxyl sulfate (0.2 and 1 mM) increases superoxide anion and nitric oxide levels in isolated human mononuclear blood cells. It increases serum creatinine and blood urea nitrogen (BUN) levels in the 5 6 nephrectomized rat model of chronic renal failure when administered at a dose of 50 mg kg.

AZ1366 is a potent tankyrase inhibitor that enhances irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance. Combination AZ1366 and irinotecan achieved greater anti-tumor effects compared to monotherapy. Activity was limited to CRC explants that displayed irinotecan resistance and increased protein levels of tankyrase and NuMA.